RU2015130950A - OXYTOCINE RECEPTOR AGONISTS FOR TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM - Google Patents

OXYTOCINE RECEPTOR AGONISTS FOR TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM Download PDF

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RU2015130950A
RU2015130950A RU2015130950A RU2015130950A RU2015130950A RU 2015130950 A RU2015130950 A RU 2015130950A RU 2015130950 A RU2015130950 A RU 2015130950A RU 2015130950 A RU2015130950 A RU 2015130950A RU 2015130950 A RU2015130950 A RU 2015130950A
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pyrazol
pyridin
benzene sulfonamide
trifluoromethylbenzenesulfonamide
chloro
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RU2664705C2 (en
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Катерина БИССАНЦ
Кристоф ГРУНДШОБЕР
Маттиас НЕТТЕКОФЕН
Жан-Марк ПЛАНШЕР
Вальтер ВИФИАН
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Ф. Хоффманн-Ля Рош Аг
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Claims (110)

1. Применение соединения формулы1. The use of the compounds of formula
Figure 00000001
,
Figure 00000001
, гдеWhere А1 представляет собой фенил или пяти- или шестичленную гетероарильную группу, содержащую 1, 2 или 3 гетероатома, выбранных из N или S;And 1 represents phenyl or a five- or six-membered heteroaryl group containing 1, 2 or 3 heteroatoms selected from N or S; R1 представляет собой водород, низший алкил, галоген, низший алкил, замещенный галогеном или циклоалкилом;R 1 represents hydrogen, lower alkyl, halogen, lower alkyl substituted with halogen or cycloalkyl; А2 представляет собой фенил;And 2 represents phenyl; R2 представляет собой галоген, низший алкил, низший алкил, замещенный галогеном, низшую алкоксигруппу, замещенную галогеном, цианогруппу, S-низший алкил, замещенный галогеном, S(O)2-низший алкил, замещенный галогеном;R 2 represents halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy group substituted by halogen, cyano group, S-lower alkyl substituted by halogen, S (O) 2 lower alkyl substituted by halogen; n равно 1 или 2;n is 1 or 2; или его фармацевтически приемлемой соли присоединения кислоты, рацемической смеси или его соответствующего энантиомера и/или его оптических изомеров для лечения аутизма, стресса, включая посттравматическое стрессовое расстройство, тревожности, включая тревожные расстройства и депрессию, шизофрении, психических расстройств и потери памяти, алкогольной абстиненции, наркозависимости, и для лечения синдрома Прадера-Вилли.or its pharmaceutically acceptable acid addition salt, racemic mixture, or its corresponding enantiomer and / or its optical isomers for treating autism, stress, including post-traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, mental disorders and memory loss, alcohol withdrawal, addiction, and for the treatment of Prader-Willi syndrome. 2. Применение соединения формулы I по п. 1 для изготовления лекарственного средства для лечения аутизма, стресса, включая посттравматическое стрессовое расстройство, тревожности, включая тревожные расстройства и депрессию, шизофрении, психических расстройств и потери памяти, алкогольной абстиненции, наркозависимости и для лечения синдрома Прадера-Вилли.2. The use of the compounds of formula I according to claim 1 for the manufacture of a medicament for the treatment of autism, stress, including post-traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, mental disorders and memory loss, alcohol withdrawal, drug dependence and for the treatment of Prader’s syndrome - Willie. 3. Применение соединения формулы I по любому из пп. 1 или 2, которое представляет собой3. The use of the compounds of formula I according to any one of paragraphs. 1 or 2, which is 4-хлор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-chloro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) -benzenesulfonamide N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметилбензолсульфонамидN- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylbenzenesulfonamide 4-этил-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-ethyl-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide 4-пропил-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-propyl-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide 2-хлор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметилбензолсульфонамид2-chloro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylbenzenesulfonamide 4-дифторметокси-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-difluoromethoxy-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide 4-хлор-N-[2-(4-фторфенил)-2Н-пиразол-3-ил]-бензолсульфонамид4-chloro-N- [2- (4-fluorophenyl) -2H-pyrazol-3-yl] benzene sulfonamide 4-циано-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-cyano-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide N-[2-(4-метилтиазол-2-ил)-2Н-пиразол-3-ил]-4-трифторметилбензолсульфонамидN- [2- (4-methylthiazol-2-yl) -2H-pyrazol-3-yl] -4-trifluoromethylbenzenesulfonamide 4-хлор-N-[2-(4-метилтиазол-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-chloro-N- [2- (4-methylthiazol-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide 4-этил-N-[2-(4-метилтиазол-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-ethyl-N- [2- (4-methylthiazol-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide N-(2-пиримидин-2-ил-2Н-пиразол-3-ил)-4-трифторметилбензолсульфонамидN- (2-pyrimidin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylbenzenesulfonamide 2,4-дихлор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид2,4-Dichloro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide 4-хлор-2-фтор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-chloro-2-fluoro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide 4-(1-фторэтил)-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4- (1-fluoroethyl) -N- (2-pyridin-2-yl-2H-pyrazol-3-yl) -benzenesulfonamide N-[2-(4-метилпиридин-2-ил)-2Н-пиразол-3-ил]-4-трифторметилбензолсульфонамидN- [2- (4-methylpyridin-2-yl) -2H-pyrazol-3-yl] -4-trifluoromethylbenzenesulfonamide 4-хлор-N-[2-(4-метилпиридин-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-chloro-N- [2- (4-methylpyridin-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide 4-этил-N-[2-(4-метилпиридин-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-ethyl-N- [2- (4-methylpyridin-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide 4-циано-N-[2-(4-метилпиридин-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-cyano-N- [2- (4-methylpyridin-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметилсульфанилбензолсульфонамидN- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylsulfanylbenzenesulfonamide 4-трифторметил-N-[2-(2-трифторметилпиримидин-4-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-trifluoromethyl-N- [2- (2-trifluoromethylpyrimidin-4-yl) -2H-pyrazol-3-yl] benzene sulfonamide 2-фтор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметилбензолсульфонамид2-fluoro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylbenzenesulfonamide N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметансульфонилбензолсульфонамидN- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethanesulfonylbenzenesulfonamide 3-фтор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметилбензолсульфонамид3-fluoro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylbenzenesulfonamide N-[2-(3-циклопропил-[1,2,4]тиадиазол-5-ил)-2Н-пиразол-3-ил]-4-этилбензолсульфонамид иN- [2- (3-cyclopropyl- [1,2,4] thiadiazol-5-yl) -2H-pyrazol-3-yl] -4-ethylbenzenesulfonamide and 4-хлор-2-фтор-N-[2-(4-метилтиазол-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид.4-chloro-2-fluoro-N- [2- (4-methylthiazol-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide. 4. Способ лечения аутизма, стресса, включая посттравматическое стрессовое расстройство, тревожности, включая тревожные расстройства и депрессию, шизофрении, психических расстройств и потери памяти, алкогольной абстиненции, наркозависимости, и для лечения синдрома Прадера-Вилли, включающий введение эффективного количества соединения формулы I.4. A method for treating autism, stress, including post-traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, mental disorders and memory loss, alcohol withdrawal, drug dependence, and for treating Prader-Willi syndrome, comprising administering an effective amount of a compound of formula I. 5. Фармацевтическая композиция, включающая соединение формулы I, выбранное из группы, состоящей из следующих соединений:5. A pharmaceutical composition comprising a compound of formula I selected from the group consisting of the following compounds: 4-хлор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-chloro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) -benzenesulfonamide N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметилбензолсульфонамидN- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylbenzenesulfonamide 4-этил-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-ethyl-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide 4-пропил-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-propyl-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide 2-хлор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметилбензолсульфонамид2-chloro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylbenzenesulfonamide 4-дифторметокси-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-difluoromethoxy-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide 4-хлор-N-[2-(4-фторфенил)-2Н-пиразол-3-ил]-бензолсульфонамид4-chloro-N- [2- (4-fluorophenyl) -2H-pyrazol-3-yl] benzene sulfonamide 4-циано-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-cyano-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide N-[2-(4-метилтиазол-2-ил)-2Н-пиразол-3-ил]-4-трифторметилбензолсульфонамидN- [2- (4-methylthiazol-2-yl) -2H-pyrazol-3-yl] -4-trifluoromethylbenzenesulfonamide 4-хлор-N-[2-(4-метилтиазол-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-chloro-N- [2- (4-methylthiazol-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide 4-этил-N-[2-(4-метилтиазол-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-ethyl-N- [2- (4-methylthiazol-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide N-(2-пиримидин-2-ил-2Н-пиразол-3-ил)-4-трифторметилбензолсульфонамидN- (2-pyrimidin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylbenzenesulfonamide 2,4-дихлор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид2,4-Dichloro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide 4-хлор-2-фтор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-chloro-2-fluoro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide 4-(1-фторэтил)-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4- (1-fluoroethyl) -N- (2-pyridin-2-yl-2H-pyrazol-3-yl) -benzenesulfonamide N-[2-(4-метилпиридин-2-ил)-2Н-пиразол-3-ил]-4-трифторметилбензолсульфонамидN- [2- (4-methylpyridin-2-yl) -2H-pyrazol-3-yl] -4-trifluoromethylbenzenesulfonamide 4-хлор-N-[2-(4-метилпиридин-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-chloro-N- [2- (4-methylpyridin-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide 4-этил-N-[2-(4-метилпиридин-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-ethyl-N- [2- (4-methylpyridin-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide 4-циано-N-[2-(4-метилпиридин-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-cyano-N- [2- (4-methylpyridin-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметилсульфанилбензолсульфонамидN- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylsulfanylbenzenesulfonamide 4-трифторметил-N-[2-(2-трифторметилпиримидин-4-ил)-2H-пиразол-3-ил]-бензолсульфонамид4-trifluoromethyl-N- [2- (2-trifluoromethylpyrimidin-4-yl) -2H-pyrazol-3-yl] benzene sulfonamide 2-фтор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметилбензолсульфонамид2-fluoro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylbenzenesulfonamide N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметансульфонилбензолсульфонамидN- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethanesulfonylbenzenesulfonamide 3-фтор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметилбензолсульфонамид3-fluoro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylbenzenesulfonamide N-[2-(3-циклопропил-[1,2,4]тиадиазол-5-ил)-2Н-пиразол-3-ил]-4-этилбензолсульфонамид иN- [2- (3-cyclopropyl- [1,2,4] thiadiazol-5-yl) -2H-pyrazol-3-yl] -4-ethylbenzenesulfonamide and 4-хлор-2-фтор-N-[2-(4-метилтиазол-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид,4-chloro-2-fluoro-N- [2- (4-methylthiazol-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide, и терапевтически инертный носитель.and a therapeutically inert carrier. 6. Соединение формулы I, раскрытое в п. 1, представляющее собой:6. The compound of formula I disclosed in paragraph 1, which represents: 4-хлор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-chloro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) -benzenesulfonamide N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметилбензолсульфонамидN- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylbenzenesulfonamide 4-этил-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-ethyl-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide 4-пропил-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-propyl-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide 2-хлор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметилбензолсульфонамид2-chloro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylbenzenesulfonamide 4-дифторметокси-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-difluoromethoxy-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide 4-хлор-N-[2-(4-фторфенил)-2Н-пиразол-3-ил]-бензолсульфонамид4-chloro-N- [2- (4-fluorophenyl) -2H-pyrazol-3-yl] benzene sulfonamide 4-циано-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-cyano-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide N-[2-(4-метилтиазол-2-ил)-2Н-пиразол-3-ил]-4-трифторметилбензолсульфонамидN- [2- (4-methylthiazol-2-yl) -2H-pyrazol-3-yl] -4-trifluoromethylbenzenesulfonamide 4-хлор-N-[2-(4-метилтиазол-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-chloro-N- [2- (4-methylthiazol-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide 4-этил-N-[2-(4-метилтиазол-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-ethyl-N- [2- (4-methylthiazol-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide N-(2-пиримидин-2-ил-2Н-пиразол-3-ил)-4-трифторметилбензолсульфонамидN- (2-pyrimidin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylbenzenesulfonamide 2,4-дихлор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид2,4-Dichloro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide 4-хлор-2-фтор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4-chloro-2-fluoro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) benzene sulfonamide 4-(1-фторэтил)-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-бензолсульфонамид4- (1-fluoroethyl) -N- (2-pyridin-2-yl-2H-pyrazol-3-yl) -benzenesulfonamide N-[2-(4-метилпиридин-2-ил)-2Н-пиразол-3-ил]-4-трифторметилбензолсульфонамидN- [2- (4-methylpyridin-2-yl) -2H-pyrazol-3-yl] -4-trifluoromethylbenzenesulfonamide 4-хлор-N-[2-(4-метилпиридин-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-chloro-N- [2- (4-methylpyridin-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide 4-этил-N-[2-(4-метилпиридин-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-ethyl-N- [2- (4-methylpyridin-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide 4-циано-N-[2-(4-метилпиридин-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-cyano-N- [2- (4-methylpyridin-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметилсульфанилбензолсульфонамидN- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylsulfanylbenzenesulfonamide 4-трифторметил-N-[2-(2-трифторметилпиримидин-4-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-trifluoromethyl-N- [2- (2-trifluoromethylpyrimidin-4-yl) -2H-pyrazol-3-yl] benzene sulfonamide 2-фтор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметилбензолсульфонамид2-fluoro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylbenzenesulfonamide N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметансульфонилбензолсульфонамидN- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethanesulfonylbenzenesulfonamide 3-фтор-N-(2-пиридин-2-ил-2Н-пиразол-3-ил)-4-трифторметилбензолсульфонамид3-fluoro-N- (2-pyridin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylbenzenesulfonamide N-[2-(3-циклопропил-[1,2,4]тиадиазол-5-ил)-2Н-пиразол-3-ил]-4-этилбензолсульфонамид иN- [2- (3-cyclopropyl- [1,2,4] thiadiazol-5-yl) -2H-pyrazol-3-yl] -4-ethylbenzenesulfonamide and 4-хлор-2-фтор-N-[2-(4-метилтиазол-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид.4-chloro-2-fluoro-N- [2- (4-methylthiazol-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide. 7. Соединение формулы IA7. The compound of formula IA
Figure 00000002
,
Figure 00000002
, гдеWhere А1 представляет собой тиазолил, пиримидинил или 1,2,4-тиадиазолил;A 1 is thiazolyl, pyrimidinyl or 1,2,4-thiadiazolyl; R1 представляет собой водород, низший алкил, галоген, низший алкил, замещенный галогеном или циклоалкилом;R 1 represents hydrogen, lower alkyl, halogen, lower alkyl substituted with halogen or cycloalkyl; А2 представляет собой фенил;And 2 represents phenyl; R2 представляет собой галоген, низший алкил, низший алкил, замещенный галогеном, низшую алкоксигруппу, замещенную галогеном, цианогруппу, S-низший алкил, замещенный галогеном, S(O)2-низший алкил, замещенный галогеном;R 2 represents halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy group substituted by halogen, cyano group, S-lower alkyl substituted by halogen, S (O) 2 lower alkyl substituted by halogen; n равно 1 или 2;n is 1 or 2; или его фармацевтически приемлемая соль присоединения кислоты, рацемическая смесь или его соответствующий энантиомер и/или его оптические изомеры.or a pharmaceutically acceptable acid addition salt thereof, a racemic mixture or its corresponding enantiomer and / or its optical isomers. 8. Соединение формулы IA по п. 7, представляющее собой:8. The compound of formula IA according to claim 7, which represents: N-[2-(4-метилтиазол-2-ил)-2Н-пиразол-3-ил]-4-трифторметилбензолсульфонамидN- [2- (4-methylthiazol-2-yl) -2H-pyrazol-3-yl] -4-trifluoromethylbenzenesulfonamide 4-хлор-N-[2-(4-метилтиазол-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-chloro-N- [2- (4-methylthiazol-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide 4-этил-N-[2-(4-метилтиазол-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-ethyl-N- [2- (4-methylthiazol-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide N-(2-пиримидин-2-ил-2Н-пиразол-3-ил)-4-трифторметилбензолсульфонамидN- (2-pyrimidin-2-yl-2H-pyrazol-3-yl) -4-trifluoromethylbenzenesulfonamide 4-трифторметил-N-[2-(2-трифторметилпиримидин-4-ил)-2Н-пиразол-3-ил]-бензолсульфонамид4-trifluoromethyl-N- [2- (2-trifluoromethylpyrimidin-4-yl) -2H-pyrazol-3-yl] benzene sulfonamide N-[2-(3-циклопропил-[1,2,4]тиадиазол-5-ил)-2Н-пиразол-3-ил]-4-этилбензолсульфонамид илиN- [2- (3-cyclopropyl- [1,2,4] thiadiazol-5-yl) -2H-pyrazol-3-yl] -4-ethylbenzenesulfonamide or 4-хлор-2-фтор-N-[2-(4-метилтиазол-2-ил)-2Н-пиразол-3-ил]-бензолсульфонамид.4-chloro-2-fluoro-N- [2- (4-methylthiazol-2-yl) -2H-pyrazol-3-yl] benzene sulfonamide.
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